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LGK974

Catalog No. T2618Cas No. 1243244-14-5
Alias WNT974, NVP-LGK974, LGK-974, LGK 974

LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.

LGK974

LGK974

Purity: 100%
Catalog No. T2618Alias WNT974, NVP-LGK974, LGK-974, LGK 974Cas No. 1243244-14-5
LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
Pack SizePriceAvailabilityQuantity
1 mg$41In Stock
2 mg$59In Stock
5 mg$97In Stock
10 mg$167In Stock
25 mg$319In Stock
50 mg$573In Stock
100 mg$819In Stock
1 mL x 10 mM (in DMSO)$97In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck.
Targets&IC50
Porcn:0.4 nM
In vitro
In both the MMTV-WNT1 mouse model of breast carcinoma and the human head and neck squamous cell carcinoma model (hn30), LGK-974 (3 mg/kg) inhibits the Wnt signaling pathway, leading to tumor regression without affecting mouse body weight. Additionally, LGK-974 (5 mg/kg, twice daily, orally) also suppresses the growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2).
In vivo
LGK-974 inhibits a range of tested Wnts, with IC50 values between 0.05 to 2.4 nM. In the PORCN radioligand binding assay, LGK-974 effectively displaces [3H]GNF-1331 with an IC50 of 1 nM and exhibits minimal cytotoxicity at 20 μM. It specifically inhibits the growth of RNF43 mutant cell lines HPAF-II, PaTu 8988S, and Capan-2.
Kinase Assay
Radioligand binding assay: using the aforementioned membrane preps, filtration binding assays are performed. To reduce nonspecific binding, 96-well filtration plates are precoated as suggested by the manufacturer with 0.1% BSA and then washed four times with 0.1% BSA. Membrane preps (50 μg total protein) are incubated in polypropylene 96-well plates with 6.6 nM 3H-GNF-1331 in the presence or absence of a testing compound in binding buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 0.1% BSA) plus EDTA-free protease inhibitor mixture in a final volume of 150 μL for 3 h at room temperature. Binding reaction mixtures are then transferred to the precoated 96-well filtration plates, filtered, and washed using a 96-pin FilterMate Harvester. Radioactive signals are obtained using a Microplate Scintillation Counter TopCount. Curve fitting is performed using Prism[1].
Cell Research
Cells are plated in growth medium in a 96-well plate at a density of 6,000–12,000 cells per well and treated with DMSO or 1 μM LGK974. After 3 d, the cells are treated with fresh growth medium containing 20 μM EdU, which is included in the Click-iT EdU Alexa Fluor 488 HCS assay kit, and the plate was incubated for 2 h at 37 °C in a humidi?ed atmosphere containing 5% CO2. Cells are ?xed with ?nal 4% (mass/vol) paraformaldehyde for 30 min, washed with PBS, permeabilized, and stained with 50 μg/mL Hoechst in PBS for 30 min. After wash, the cells are proceeded to EdU detection according to the instruction of Click-iT EdU assay kit. Triplet wells are performed for each condition. (Only for Reference)
AliasWNT974, NVP-LGK974, LGK-974, LGK 974
Chemical Properties
Molecular Weight396.44
FormulaC23H20N6O
Cas No.1243244-14-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 73 mg/mL (184.1 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5224 mL12.6122 mL25.2245 mL126.1225 mL
5 mM0.5045 mL2.5224 mL5.0449 mL25.2245 mL
10 mM0.2522 mL1.2612 mL2.5224 mL12.6122 mL
20 mM0.1261 mL0.6306 mL1.2612 mL6.3061 mL
50 mM0.0504 mL0.2522 mL0.5045 mL2.5224 mL
100 mM0.0252 mL0.1261 mL0.2522 mL1.2612 mL

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